| Description | Tanomastat is an orally bioavailable and non-peptidic biphenyl matrix metalloproteinases inhibitor. For MMP-2, MMP-3, MMP-9, MMP-13 the Ki values are 11, 143, 301, and 1470 nM respectively. |
| In vitro | Tanomastat (1-00 μM; 5 days) inhibits tubule formation completely at 15-100 μM. Tanomastat (1-10000 nM; 6 hours) prevents matrix invasion by endothelial cells in a concentration-dependent manner (IC50=840 nM) [2][3]. |
| In vivo | Tanomastat (100 mg/kg; p.o.; daily for a 7-week period) inhibits local tumor regrowth and inhibits the number and volume of lung metastases [3]. |
| Target activity | MMP2:11 nM （ki）, MMP13:1470 nM （ki）, MMP9:301 nM （ki）, MMP3:143 nM （ki） |
| Synonyms | BAY 12-9566 |
| molecular weight | 410.91 |
| Molecular formula | C23H19ClO3S |
| CAS | 179545-77-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Leung D, et al. Protease inhibitors: current status and future prospects. J Med Chem. 2000 Feb 10;43(3):305-41. 2. Gatto C, et al. BAY 12-9566, a novel inhibitor of matrix metalloproteinases with antiangiogenic activity. Clin Cancer Res. 1999 Nov;5(11):3603-7. 3. Nozaki S, et al. Activity of biphenyl matrix metalloproteinase inhibitor BAY 12-9566 in a human breast cancerorthotopic model. Clin Exp Metastasis. 2003;20(5):407-12. |